Skeletal Muscle Relaxants Flashcards
Neuromuscular blockers
Block at nicotinic receptors
-Competitive non depolarizing
-Depolarizing
Spasmolytic drugs
Centrally acting - Backofen diazepam
Direct - Dantrolene
Others
Inhibit synthesis
Inhibit release
Inhibit storage
Synthesis
Hemicholinium
Triethylcholine
Inhibit release
++Mg –Ca
Local anaesthetic like procaine
Botulinum toxin
Inhibit storage (in vmVESicles(
Vesamicol
Botulinum used in
Ocular blepharospasm and strabismus
Oesophagus achalasia
Generalised spastic disorders like cerebral palsy
Overactive bladder
Neuromuscular blocking (poorly lipid soluble so tiny CNS) plus inactive orally so parenteral)
Larger muscles are more resistant and recover rapidly
Diaphragm is the last
Atracurium
Hofmann(spontaneous)elimination
With NO effect on muscarinic receptors and slight histamine release
Cisatracium
Mostly spontaneous release
With NO effect on muscarinic receptors and NO histamine release
TuboCURARine - prototype
It and atracurium cause hypotension
Kidney elimination with NO effect on cardiac muscke and MODERATE histamine release
Panacuronium
Kidney elimination With MODERATE blockade of muscarinic receptors and NO histamine release
*Tachycardia
Rocuronoum - least potent, fastest onset and rapid action
Liver and Kidney elimination With SLIGHT effect on muscarinic and NO histamine release
*Yet it has allergic reactions
Sugammadex
Forms complex with rocuronium to get it away from NM junction
Local anaesthetics causing depression, increasing blood flow and decreasing the sensitivity of the postjunctional membrane to depolaridation from best to worst
Isoflurane, sevoflurane, halothane and nitric oxide
Higher doses of local anaesthetics
Block nicotinic receptors
Antibiotic synergism
Aminoglycosides
Antiarrhythmic synergism - class 2
Quinidine
Does myasthenia gravis count as a synergist?
Yes
Advanced ages as a synergist?
Yes
Decreased clearance of drugs
Decreased Neuromuscular blockade
Anticholine esterases
Sugammadex - no rocuronium and rancuronium
Burns
UMNL
Depolarizing agents
Succinylchoiline causing unresponsive depolarization in phase 1 - block
Prolonged exposure causing desensitisation in phase 2
Hydrolysis of succinylcholine
Butyrylcholine - liver
Pseudocholine - plasma
Side effects of succinyl
Arrhythmia and bradycardia
Respiratory apnea - fresh frozen blood for phase 1
Malignant hyperthermia because of anaesthetics and the succinyl
*treat with dantrolene
Hyperkalemia
Centrally actingnspasmolytic drugs
Diazepam at GABA A synapses
Baclofen - drowsiness with eventual tolerance
And agonist at GABA B
*reduces pain by inhibiting substance p
Substance p
Neurokinin1
TizAnidine
Alpha 2 Adrenoceptor
Causing hypotension drowsiness and dry mouth
Gabapentin
Antiepileptic spasmolytic in MS
Newer Gabapentin
Pregabalin
Direct
Dantrolene through Ryr inhibition so no calcium
IV or ORAL